BICYCLIC HETEROAROMATIC COMPOUNDS AS LH AGONISTS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

Abstract RU 2248979 C2

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to a new derivative of bicyclic heteroaromatic compound of the general formula (I) or its pharmaceutically acceptable salt eliciting agonistic activity with respect to luteinizing hormone (LH). Compounds can be used for preparing medicinal agents for control ability for conception. In compounds of the general formula (I) R1 represents R7 wherein R7 represents (C6-C10)-aryl optionally substituted with halogen atom at ortho- and/or meta-position; NHR8, OR8 wherein R8 means (C1-C8)-alkyl that can be substituted with halogen atom, (C1-C8)-alkylcarbonyl, (C1-C8)-alkylcarbonyloxy-group, phenyl, (C6-C10)-arylcarbonylamino-group, 5-methyl-2-phenylimidazol-4-yl, (C6)-heterocycloalkyl wherein 1-2 heteroatoms are taken among nitrogen and oxygen atoms, ethyloxycarbonylmethylthio-(C1-C4)-alkoxy-group, amino-group, (C6-C7)-heteroaryl; or (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; R2 represents (C1-C8)-alkyl or (C6-C10)-aryl optionally substituted with one or more substitutes taken among (C1-C8)-alkoxy-group; or (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; R3 represents (C1-C8)-alkyl possibly substituted with (C6-C14)-aryl possibly substituted with halogen atom, (C1-C4)-alkoxy-group, (C1-C4)-alkoxycarbonyl, mono- or tri-(C6-C10)-cycloalkyl, (C6-C10)-aryl, (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; (C5-C7)-heterocycloalkyl comprising 2 heteroatoms taking among nitrogen or oxygen atom; (C3-C8)-cycloalkyl, (C2-C7)-heterocycloalkyl comprising 2 heteroatoms taking among nitrogen or oxygen atom; or (C6-C10)-aryl optionally substituted with one or more substitutes taken among (C1-C8)-alkoxy-group; X represents sulfur atom (S) or N(R4); Y represents nitrogen atom (N); R4 represents (C1-C8)-alkyl, phenyl-(C1-C8)-alkyl; or X represents sulfur atom (S), and Y represents CH; Z represents NH2 or OH; A represents sulfur (S), oxygen atom (O) or a bond. Also, invention relates to a pharmaceutical composition.

EFFECT: valuable properties of compounds and composition.

14 cl, 1 tbl, 119 ex

Similar patents RU2248979C2

Title Year Author Number
GLYCINE-SUBSTITUTED THIENO[2,3-D]PYRIMIDINES WITH COMBINED LH- AND FSH-AGONISTIC ACTIVITY 2002
  • Khanssen Robert Gerard Jules Mari
  • Timmers Kornelis Marius
  • Kelder Jan
RU2294331C2
DERIVATIVES OF THIENO[2,3-D]PYRIMIDINE AND THEIR USING IN TREATMENT OF FERTILITY DISORDER 2002
  • Khanssen Robert Gerard Jules Mari
  • Timmers Kornelis Marius
RU2298011C2
BICYCLIC HETEROAROMATIC COMPOUNDS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND USING 2001
  • Timmers Kornelis Marius
  • Karstens Villem Frederik Jokhan
RU2271360C2
SUBSTITUTED PYRIMIDINETHIOALKYL OR ALKYLESTER COMPOUNDS AND METHOD OF INHIBITION OF VIRAL REVERSE TRANSCRIPTASE ACTIVITY 1996
  • Richard A. N'Judzhent
  • Donn G. Vishka
  • Gari Dzh. Klik
  • Dehvid R. Grejber
  • Stiven Tomas Shljakhter
  • Majkl Dzh. Merfi
  • Dzhoel Morris
  • Richard S. Tomas
RU2167155C2
SERINE PROTEASE INHIBITOR AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1999
  • Timmers Kornelis Marius
  • Revinkel Jokhannes Bernardus Marija
RU2232760C2
BICYCLICAL NITROGEN-CONTAINING HETEROCYCLES AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF 1999
  • Kharris Uill'Jam
  • Khill Kristofer Khu
  • Smit Ajan Ehduard Dejvid
RU2256662C2
BRK INHIBITING COMPOUND 2016
  • Yamamoto, Shingo
  • Tokura, Hiroshi
  • Kurono, Masakuni
  • Nomura, Yoshinori
  • Hotta, Shingo
RU2719477C2
METHODS AND INTERMEDIATE COMPOUNDS FOR PREPARING IMATINIB, OPTIONALLY RADIOLABELLED 2006
  • Salter Ris
  • Rodriges-Peres Marija-Ines
  • Menius Tomas
  • Foges Rol'F
  • Andres Khendrik
  • Bordo Kirk
RU2440999C2
THIENOPYRIMIDINE DERIVATIVES, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND METHOD FOR ANTAGONIZATION OF GONADOTROPIN-RELEASING HORMONE 2000
  • Furuja Suiti
  • Suzuki Nobukhiro
  • Tokh Nobuo
  • Nara Josi
RU2233284C2
THIENOPYRIMIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION 1994
  • Suiti Furuja
  • Nobuo Tokh
  • Tetsuja Okhtaki
  • Tosifumi Vatanabe
RU2142275C1

RU 2 248 979 C2

Authors

Gerritsma Gerrildina Gezina

Van Straten Nikol' Korin Rene

Adang Anton Ehgbert Peter

Dates

2005-03-27Published

2000-04-03Filed